AR093818A1 - Compuesto de 1-(bencil sustituido)piperazina sustituida - Google Patents
Compuesto de 1-(bencil sustituido)piperazina sustituidaInfo
- Publication number
- AR093818A1 AR093818A1 ARP130104518A ARP130104518A AR093818A1 AR 093818 A1 AR093818 A1 AR 093818A1 AR P130104518 A ARP130104518 A AR P130104518A AR P130104518 A ARP130104518 A AR P130104518A AR 093818 A1 AR093818 A1 AR 093818A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- phenyl
- optionally substituted
- group
- substituted
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/16—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Abstract
Un compuesto de 1-(bencil sustituido)piperazina sustituida, o una de sus sales farmacéuticamente aceptables, que es de la fórmula (1) en donde: R¹ es: alquilo C₁₋₆; metilo sustituido con i) cicloalquilo C₃₋₅; ii) fenoxi; o iii) un fenilo y un segundo sustituyente seleccionado del grupo que consiste en: metilo halo y metoxi; etilo sustituido con i) fenilo, dicho fenilo está opcionalmente sustituido con halo o metoxi o ii) heteroarilo; bencilo, en donde el grupo fenilo de dicho bencilo está opcionalmente sustituido con halo, metoxi o SO₂CH₂CH₃; alquenilo C₂ opcionalmente sustituido con un F y un fenilo; cicloalquilo C₃₋₇, dicho cicloalquilo está opcionalmente sustituido con uno o dos sustituyentes seleccionados del grupo que consiste en fenilo, metilo y F; o dicho cicloalquilo está opcionalmente fusionado con un anillo fenilo; heterocicloalquilo opcionalmente sustituido con uno o dos alquilo C₁₋₃; heteroarilo opcionalmente sustituido con uno a dos sustituyentes seleccionados del grupo que consiste en: alquilo C₁₋₃, alcoxi C₁₋₃ y CF₃; y fenilo sustituido con uno a tres sustituyentes seleccionados del grupo que consiste en: i) halo; ii) CN; iii) alquilo C₁₋₃ opcionalmente sustituido con uno a tres F; iv) alcoxi C₁₋₃; v) (CH₂)ₙNRᵃRᵇ; vi) C(O)CH₃; y vii) CH₂OCH₃; R² es halo o alquilo C₁₋₃; R³ es halo o metilo; R⁴ es H o metilo; R⁵ es alquilo C₁₋₃; R⁶ es alquilo C₁₋₃; R⁷ está seleccionado del grupo que consiste en: alquilo C₁₋₇ opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en halo, cicloalquilo C₃₋₅ y CF₃; cicloalquilo C₃₋₇ opcionalmente sustituido con uno o dos sustituyentes seleccionados del grupo que consiste en F, CH₂F, CHF₂, metilo y metoxi; cada k es 0 ó 1; cada p 0 ó 1; cada n es 0, 1 ó 2; cada Rᵃ es H o alquilo C₁₋₃; cada Rᵇ es H o alquilo C₁₋₃; siempre que: (i) R⁷ no sea fenilo cuando R¹ es piperazinilo; y ii) R⁷ no sea clorofenilo cuando R¹ es fenilo. Estos compuestos son moduladores del receptor huérfano g relacionado con retinoides (RORg) y se emplean en el tratamiento de enfermedades mediadas por RORg.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012001636 | 2012-12-06 | ||
| CN2013000182 | 2013-02-25 | ||
| CN2013000803 | 2013-07-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR093818A1 true AR093818A1 (es) | 2015-06-24 |
Family
ID=49709687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104518A AR093818A1 (es) | 2012-12-06 | 2013-12-05 | Compuesto de 1-(bencil sustituido)piperazina sustituida |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US10005731B2 (es) |
| EP (2) | EP2928885B1 (es) |
| JP (1) | JP6279605B2 (es) |
| KR (1) | KR20150092244A (es) |
| CN (1) | CN105121430B (es) |
| AR (1) | AR093818A1 (es) |
| AU (1) | AU2013354109B2 (es) |
| BR (1) | BR112015013137B1 (es) |
| CA (1) | CA2894016C (es) |
| CL (1) | CL2015001557A1 (es) |
| CR (1) | CR20150302A (es) |
| CY (1) | CY1118932T1 (es) |
| DK (1) | DK2928885T3 (es) |
| EA (1) | EA026437B1 (es) |
| ES (1) | ES2626390T3 (es) |
| HK (1) | HK1214814A1 (es) |
| HR (1) | HRP20170638T1 (es) |
| HU (1) | HUE033212T2 (es) |
| IL (1) | IL239082A0 (es) |
| LT (1) | LT2928885T (es) |
| ME (1) | ME02696B (es) |
| MX (1) | MX2015007180A (es) |
| PE (1) | PE20151144A1 (es) |
| PH (1) | PH12015501244A1 (es) |
| PL (1) | PL2928885T3 (es) |
| PT (1) | PT2928885T (es) |
| RS (1) | RS55875B1 (es) |
| SG (1) | SG11201504200TA (es) |
| SI (1) | SI2928885T1 (es) |
| SM (1) | SMT201700281T1 (es) |
| TW (1) | TW201427959A (es) |
| UY (1) | UY35174A (es) |
| WO (1) | WO2014086894A1 (es) |
| ZA (1) | ZA201503666B (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6192836B2 (ja) * | 2013-07-30 | 2017-09-06 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｒｏｒｃモジュレーターとしてのアザインドール化合物 |
| MX371017B (es) | 2014-02-03 | 2020-01-13 | Vitae Pharmaceuticals Llc | Inhibidores de dihidropirrolopiridina de receptor huerfano relacionado-gamma. |
| BR112016027732B1 (pt) * | 2014-05-28 | 2023-11-07 | Glaxosmithkline Intellectual Property Development Limited | Composto modulador do receptor gama, composição farmacêutica que compreende o referido composto, bem como uso do mesmo para o tratamento de doenças inflamatórias e autoimunes mediadas por rory |
| CN106660999A (zh) | 2014-05-28 | 2017-05-10 | 葛兰素史密斯克莱知识产权发展有限公司 | 新化合物 |
| SG11201609722UA (en) * | 2014-05-28 | 2016-12-29 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| CN104292208A (zh) * | 2014-09-09 | 2015-01-21 | 上海师范大学 | 7-苯基-6,8-二氧杂螺[3.5]壬烷-2-羧酸及其制备方法 |
| MA40759A (fr) * | 2014-09-26 | 2017-08-01 | Pfizer | Modulateurs de rorc2 de type pyrrolopyridine substitué par un méthyle et trifluorométhyle et leurs procédés d'utilisation |
| JP6564029B2 (ja) | 2014-10-14 | 2019-08-21 | ヴァイティー ファーマシューティカルズ，エルエルシー | Ｒｏｒ−ガンマのジヒドロピロロピリジン阻害剤 |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| TW201625588A (zh) * | 2014-11-05 | 2016-07-16 | 第一三共股份有限公司 | 環狀胺衍生物 |
| WO2016120849A1 (en) * | 2015-01-30 | 2016-08-04 | Pfizer Inc. | Methoxy-substituted pyrrolopyridine modulators of rorc2 and methods of use thereof |
| ES2856931T3 (es) | 2015-08-05 | 2021-09-28 | Vitae Pharmaceuticals Llc | Moduladores de ROR-gamma |
| BR112018010018A2 (pt) * | 2015-11-20 | 2018-11-21 | Vitae Pharmaceuticals Inc | moduladores de ror-gama |
| TWI757266B (zh) | 2016-01-29 | 2022-03-11 | 美商維它藥物有限責任公司 | ＲＯＲ－γ調節劑 |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| SG11201811107WA (en) * | 2016-07-13 | 2019-01-30 | Leo Pharma As | Heteroaromatic modulators of the retinoid-related orphan receptor gamma |
| CN109134476B (zh) * | 2017-06-15 | 2021-03-19 | 复旦大学 | 桥环哌嗪类衍生物或其盐及其制备方法和用途 |
| TW201908280A (zh) | 2017-07-18 | 2019-03-01 | 瑞士商隆薩有限公司 | 製備5-氟-2-甲基-3-硝基苯甲酸及其甲酯的方法 |
| EP3658555A1 (en) | 2017-07-24 | 2020-06-03 | Vitae Pharmaceuticals, LLC | Inhibitors of ror |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| CN108752185A (zh) * | 2018-07-17 | 2018-11-06 | 成都道合尔医药技术有限公司 | 一种1-氟-环戊甲酸的合成方法 |
| CN109438423A (zh) * | 2018-09-12 | 2019-03-08 | 通化师范学院 | 一种肺癌靶向化合物azd-3759的合成工艺的新方法 |
| CN110862319A (zh) * | 2019-12-04 | 2020-03-06 | 深圳振强生物技术有限公司 | 奥扎格雷杂质的制备方法 |
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| WO2023232870A1 (en) | 2022-05-31 | 2023-12-07 | Immunic Ag | Rorg/rorgt modulators for the treatment of virus infections like covid-19 |
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| US10286000B2 (en) | 2013-10-25 | 2019-05-14 | St. Jude Children's Research Hospital, Inc. | Retinoid X receptor-gamma agonists and retinoid X receptor-alpha antagonists for treatment of cancer |
| SG11201609722UA (en) | 2014-05-28 | 2016-12-29 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| CN106660999A (zh) | 2014-05-28 | 2017-05-10 | 葛兰素史密斯克莱知识产权发展有限公司 | 新化合物 |
| BR112016027732B1 (pt) | 2014-05-28 | 2023-11-07 | Glaxosmithkline Intellectual Property Development Limited | Composto modulador do receptor gama, composição farmacêutica que compreende o referido composto, bem como uso do mesmo para o tratamento de doenças inflamatórias e autoimunes mediadas por rory |
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2013
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